[논문]Sulfamoylbenzamide-based Capsid Assembly Modulators for Selective Inhibition of Hepatitis B Viral Replication

Lee, Yeon Hee; Cha, Hyeon-Min; Hwang, Jun Yeon; Park, So Yeong; Vishakantegowda, Avinash G.; Imran, Ali; Lee, Joo-Youn; Yi, Yoon-Sun; Jun, Sangmi; Kim, Ga Hyeon; Kang, Hyo Jin; Chung, Sang J.; Kim, Meehyein; Kim, Hyejin; Han, Soo Bong

doi:10.1021/acsmedchemlett.0c00606

[해외논문] Sulfamoylbenzamide-based Capsid Assembly Modulators for Selective Inhibition of Hepatitis B Viral Replication 원문보기

ACS medicinal chemistry letters, v.12 no.2, 2021년, pp.242 - 248

Lee, Yeon Hee (Therapeutics & Biotechnology Division , Korea Research Institute of Chemical Technology , Daejeon 34114 , Republic of Korea) , Cha, Hyeon-Min (Therapeutics & Biotechnology Division , Korea Research Institute of Chemical Technology , Daejeon 34114 , Republic of Korea) , Hwang, Jun Yeon (Therapeutics & Biotechnology Division , Korea Research Institute of Chemical Technology , Daejeon 34114 , Republic of Korea) , Park, So Yeong (Therapeutics & Biotechnology Division , Korea Research Institute of Chemical Technology , Daejeon 34114 , Republic of Korea) , Vishakantegowda, Avinash G. (Therapeutics & Biotechnology Division , Korea Research Institute of Chemical Technology , Daejeon 34114 , Republic of Korea) , Imran, Ali (Therapeutics & Biotechnology Division , Korea Research Institute of Chemical Technology , Daejeon 34114 , Republic of Korea) , Lee, Joo-Youn (Therapeutics & B) , Yi, Yoon-Sun , Jun, Sangmi , Kim, Ga Hyeon , Kang, Hyo Jin , Chung, Sang J. , Kim, Meehyein , Kim, Hyejin , Han, Soo Bong

Abstract ▼ AI-Helper

As the spread of infections caused by hepatitis B virus (HBV) threatens public health worldwide, investigations from multiple perspectives and of various mechanisms of action are urgently required to increase the HBV cure rate. Targeting the encapsidation of the nuclear capsid protein (core protein, HBc) has emerged as an attractive strategy for inhibiting the viral assembly process; however, a drug targeting this mechanism has not yet been approved. We synthesized novel sulfamoylbenzamides (SBAs) as capsid assembly modulators of HBV and found that the effects and safety profiles of compounds 3 and 8 have potential therapeutic applicability against HBV. The formation of tubular particles was time-dependent in the presence of 3, indicating a new mode of protein assembly by SBA compounds. Our findings provide a new entity for developing safe and efficient treatments for HBV infection.[FIG OMISSION]

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